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CAS No.: 1627503-67-6

LDN-214117 Catalog No. CSN13876

LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM with > 100 fold selectivity for ALK5, and also inhibits BMP6 (IC50=100 nM).

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The bone morphogenetic protein (BMP) signal transduction pathway is a subset of the larger TGF-β signaling family, which includes 7 type I receptors, 5 type II receptors, and over 30 ligands of the BMP, TGF-β, activin, and growth and differentiation factor (GDF) ligand families^[2]. LDN-214117 is a high degree of selectivity inhibitor for the BMP type I receptor kinase ALK2 with IC50 value of 24 nM. LDN-214117 also inhibits the activity of BMP6 and TGFβ with IC50 values of 67 nM and 14.65 μM, respectively (measured by ligand induced transcriptional assay)^[1]. In vitro, LDN-214117 inhibited ACR1 wild-type cells SU-DIPG-VI and QCTB-R059 with GI50 values of 5.38 μM and 8.27 μM, respectively. LDN-214117 also inhibited cell viability of the ACVR1 mutant cells HSJD-DIPG-007(R206H), SU-DIPG-IV(G238V) and HSJD-DIPG-018(R258G) with GI50 values of 1.57 μM, 6.23 μM and 16.38 μM, respectively. Treatment DIPG cell lines SU-DIPG-VI and HSJD-DIPG-IV with 0.1 μM LDN-214117 for 4h inhibited phosphor-SMAD1/5/8 and the downstream effector ID1^[3]. In addition, treatment the lung carcinoma cell line LCLC-103H with LDN-214117 at concentration of 5 μM significantly hindered the migration of LCLC-103H cells into the wound area, reaching relative wound density of only 50% in 48h by inhibition of BMP signaling^[4]. In vivo, the bioavailability (F) and well-tolerance level of LDN-214117 was 0.75 and 25 mg/kg, respectively. Oral administration of LD-214117 at 25 mg/kg for 28 days extended survival in immunodeprived mice bearing orthotopic xenografts of H3.3K27M, ACVR1R206H mutant HSJDDIPG-007 cells^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
C2C12 cells	-	Function assay	30 mins	Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay, IC50=0.1 μM	25101911
HEK293T cells	-	Function assay	30 mins	Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay, IC50=0.027 μM	25101911

参考文献

[1] Mohedas A H , Wang Y , Sanvitale C E , et al. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. Journal of Medicinal Chemistry, 2014, 57(19).
[2] Dinter T, Bocobo G, Yu P B, et al. Pharmacologic Strategies for Assaying BMP Signaling Function. Methods of Molecular Biology, 2019: 221-233.
[3] Carvalho D, Taylor KR, Olaciregui NG, et al. ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Commun Biol. 2019;2:156.
[4] Mihajlovic J, Diehl L A, Hochhaus A, et al. Inhibition of bone morphogenetic protein signaling reduces viability, growth and migratory potential of non-small cell lung carcinoma cells. Journal of Cancer Research and Clinical Oncology, 2019, 145(11): 2675-2687.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3837 mL
- 11.9185 mL
- 23.8370 mL
- 5 mM
- 0.4767 mL
- 2.3837 mL
- 4.7674 mL
- 10 mM
- 0.2384 mL
- 1.1918 mL
- 2.3837 mL

技术信息

CAS号

1627503-67-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H29N3O3

运输

蓝冰

分子量

419.52

别名

溶解度

DMSO	83.0 mg/mL (197.8 mM)
Water	Insoluble
Ethanol	83.0 mg/mL (197.8 mM)

动物实验配方

2% DMSO+30% PEG 300+2% Tween 80+water

3 mg/mL

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